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TASIN-1 is a small molecule inhibitor that specifically kills cells with adenomatous polyposis coli (APC) truncations (IC50 = 70 nM) but spares cells with wild-type APC.1 TASIN-1 is effective in vivo, inhibiting tumor growth of colorectal cancer (CRC) cells with truncated APC, but not wild-type CRC cells, in a mouse xenograft model.1 TASIN-1 decreases cholesterol biosynthesis in APC-truncated cells but not in wild-type APC cells.1
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1. Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer. Sci. Transl. Med. 8(361), 361ra140 (2016).